Orlistat

Learn why so many people choose Orlistat to lose weight.

If you already heard something about this medication, get the answers to frequently asked questions and check out Orlistat and cardiovascular problems, Orlistat contraindications.

If you only started your research about this weight loss drug, enjoy getting all info you need by reading further.

Why fight obesity with Orlistat

Obesity – is a chronic disease, occurring due to formation and accumulation of excessive fat tissue in the human body.

Yes, obesity can be caused by such triggers, as:

  • insufficient sleep,
  • high stress,
  • endocrine disorders,
  • genetic predisposition.

However, if we check off the abovementioned causes, the risk group of obesity includes people, who lead a sedentary lifestyle and who do not follow a normal diet.

excess weight is caused by an imbalance between incoming and expended energy throughout a day.

It means that most people with excess weight spend less energy than they consume in calories during the day.

The excess calories accumulate in the body in form of visceral and subcutaneous fat.

Excess weight increases the risk of concomitant diseases, including:

  • cardiovascular disorders,
  • gallbladder disease,
  • endocrine disorders.

In order to reduce the risk of complications, occurring with adiposity, you should keep to a well-balanced diet and make exercises.

If your weight loss attempts prove insufficient, you can try using one of the most effective and safe weight loss medication – Orlistat (gastrointestinal lipase inhibitor).

It is one of the few types of diet drugs, which successfully passed clinical trials in the US and Europe.

The drug appeared on the pharmaceutical market in 1998 and as might be expected from any new weight management strategy, rumors of his prowess were greatly exaggerated.

Orlistat fat blocker is intended for those people, who are at high risk of complications because of extra weight.

Orlistat in any case is not a panacea.

This drug works only in conjunction with well-known to everyone changes in eating and exercise.

As practice has shown, the drug Orlistat is moderately effective in treating people, who suffer from extreme obesity.

Herewith, this gastric lipase inhibitor does not to pose any serious health risks.

The Mechanism of Orlistat Action

Orlistat, the brand name of which is Xenical, blocks an enzyme required for fat digestion.

If complete blocking of fat absorption would be possible, these weight loss pills could be a dream of any obese person.

During the treatment course with Orlistat, 30 percent of fats contained in food are temporarily accumulated in the intestines, and then they are excreted undigested.

This mechanism of action prevents penetration and accumulation of fats in the body.

If we compare the action mechanism of Orlistat fat blocker with the action mechanism of appetite suppressants (e.g., Phentermine), the first has a number of advantages:

  • Orlistat does not affect the heart function, which is already weakened in the majority of obese people
  • The fat blocker does not cause physical or psychological addiction
  • Orlistat works well and very reliably, so it can be used for a long time.

Orlistat is classified as an anti-obesity drug of peripheral action.

Such mechanism of action is safer for health and at the same time is a major cause of unpleasant Orlistat side effects.

It should be noted, though, that weight loss pills Orlistat do not pose any serious health risks.

Some skeptics believe that such mechanism of action as blocking of fat absorption cannot contribute to a significant weight loss and successful treatment of obesity.

However, skilled health professionals argue that weight loss should be gradual without stress for the body’s metabolism.

From the medical point of view, a goal of obesity treatment is not achieving an ideal body weight.

Help is necessary for people to achieve biologically acceptable weight, at which they will not be at increased risk of cardiometabolic diseases.

It is worth to pay attention to another aspect.

Orlistat excretes fats from the body together with the fat-soluble vitamins.

In order to maintain a normal balance of essential substances, this weight loss drug should be taken in combination with multivitamins.

Orlistat is considered anti-obesity drug of moderate effectiveness.

However, until “magic” slimming pills appear, Orlistat will be one of the most commonly prescribed drugs for treatment of overweight or obesity.

Orlistat Properties

After the beginning of Orlistat marketing, some weight loss experts were quick to say that the fat blocker helps to lose only modest amounts of weight.

Observations made during usual medical practice have established that regular use of Orlistat helps to lose 5 to 15 percent of the initial body weight.

Weight loss by 5-15 percent is not the most outstanding results.

The same results can be achieved by means of appetite suppressants, herewith for a shorter time.

However, Orlistat has some undeniable advantages that favorably distinguish it from other weight loss pills.

Orlistat is a peripherally acting drug that works only in the intestine.

It makes one-third of fats contained in food to be excreted from the body naturally.

Orlistat does not increase blood pressure and does not affect the brain function.

History of all, without exception, appetite suppressants are accompanied with information that they often cause physical addiction and / or raise in arterial blood pressure.

During the use of Orlistat, you do not have to worry about this.

Besides, Orlistat is recommended for long-term treatment of obesity.

It is the first and only anti-obesity drug that can be an integral part of long-term weight loss program.

Effectiveness and safety of Orlistat is confirmed by national regulators, weight loss experts and consumers’ reviews, so the drug is available in more than 50 countries around the world.

Recommendations for Orlistat use

For a more effective weight loss before and during a course of Orlistat use, it is recommended to use diet and exercise.

These methods in complex help to quickly restore a proper metabolic rate.

This improves the work of vital functions and promotes weight loss.

Physical activity contributes to a fast conversion of calories into energy due to fat deposits in the body.

Due to sports therapy during Orlistat use, redox processes are also increased, while the function of cardiovascular, digestive and respiratory systems improve.

Physical activity in combination with Orlistat use considerably reduces the risk of many diseases that accompany obesity.

Among them, type 2 diabetes and diseases of the cardiovascular system, such as stroke, myocardial infarction and angina pectoris are particularly dangerous.

  • However, the drug is not intended for the prevention of such diseases.

For the maximum effectiveness of Orlistat, various methods of a balanced diet are also used.

Compliance with a balanced and hypocaloric diets helps to regulate the amount of fats, thereby fat absorption process is suspended.

Once again, we remind you that some vitamins such as A, O, D and E are cleaved only in fats.

When using Orlistat, the absorption of these fat-soluble vitamins decreases.

If you take a vitamin and mineral complex, you should not take them during the main meals.

Better take them before bedtime.

Orlistat dosing regimen

Orlistat is one of few medications, which can be prescribed for the treatment of adiposity not just in adults, but pediatric patients over 12 years old.

Children over 12 years old do not require special adjustment of Orlistat daily dose.

  • For I-II class obesity, the initial dose of Orlistat – is 60mg (one capsule of Orlistat 60mg).
  • Orlistat 60mg capsules have to be taken three times a day, before or soon after meals.
  • The intake of another dose of Orlistat 60mg can be skipped, if food does not contain fats (or you missed your meal).
  • When taking Orlistat 60mg, the foods must contain under 30% of fats, not more. The less fat you take with food, the less Orlistat side effects you will have.
  • The recommended duration of use of Orlistat 60mg capsules during the therapeutic treatment of I and II class obesity – is 6 months.
  • The maximum recommended daily dose of Orlistat for patients with I and II class obesity – is 1800mg (which is three Orlistat 60mg capsules).
  • In the treatment of III and IV degrees of obesity, Orlistat single dose is 120mg.
  • Patients with III and IV-degree obesity are recommended to take one capsule Orlistat 120mg three times a day.
  • Orlistat 120mg capsules can be taken with food, one hour before food or one hour after food.
  • In obesity treatment, the most effective result is achieved when taking Orlistat 120mg capsules in combination with low-calorie, balanced diet.
  • Food consumption, containing more than 30% of fat in combination with single dose Orlistat 120mg increases the risk of gastrointestinal side effects (diarrhea).
  • When treating of III and IV obesity degrees, recommended duration of the drug use is six month.

Orlistat inhibits fat absorption from the gastrointestinal tract, so if you skip a meal or a meal contains a minimum amount (zero) animal and vegetable fats, you can skip a single Orlistat dose.

If you forget to take a capsule, you may take it any time, if the meal took place not more than 1 hour ago.

If more than 2 hours passed after a meal, it is recommended to skip an Orlistat dose.

During this time, most of the fat, ingested with food, has been already digested by the body, and Orlistat will not provide a therapeutic effect.

Double Orlistat dose will not increase Orlistat therapeutic effect.

Compensating for the missed dose with a double Orlistat dose is not recommended.

Effectiveness of Orlistat drug

Use of maximum recommended Orlistat dosage of 120mg three times a day helps to:

  • reduce the mass of visceral and abdominal fat;
  • reduce the amount of free fatty acids and monoglycerides in the intestinal lumen;
  • reduce the ability of cholesterol to penetrate in the blood plasma;
  • increase tissue insulin sensitivity.

When treating III and IV degrees of obesity, results of clinical studies have proved that daily use of Orlistat 120mg capsules for 52 weeks contributes to:

  • weight loss by 6,2%;
  • decrease in plasma insulin level by 18%.

Therefore, Orlistat drug not only reduces excess weight but also decreases the risk of obesity-associated diseases.

Orlistat Benefits

You already know that Orlistat is the first and only inhibitor of gastric and pancreatic lipases.

This fat blocker works effectively and safely.

Due to its distinctive features, Orlistat can compete with anti-obesity drug Phentermine, which is a recognized sales leader in the United States for many decades.

The main advantages of Orlistat are:

  • Sustained weight loss and reduction of unwanted inches
  • Lack of cardiovascular side effects
  • The FDA approval as part of long-term weight loss program.

Before Orlistat (Xenical) has received the FDA approval in 1999, many people had contraindications to drug therapy of overweight or obesity.

The fact that the central nervous system stimulants do not only suppress appetite, but also raise blood pressure and pulse rate.

This specific inhibitor of lipases operates in the gastrointestinal tract and has no effect on other body systems.

Therefore, people with cardiovascular diseases can take Orlistat without increasing risk of severe cerebral circulation impairment and irreversible necrosis of heart muscle.

The main advantage of Orlistat is that this fat blocker is approved for long-term treatment of overweight or obesity.

Prescription appetite suppressants should be taken no more than 12 weeks that explains high failure rate among people using this type of anti-obesity drugs

This fat blocker does not cause physical or psychological addiction, so people suffering from obesity can buy low doses of Orlistat (Alli) without prescription.

The drug has a good cost-effectiveness ratio, eliminates risk of adverse effects and therefore has a great potential for successful weight loss.

Popular Orlistat Brands

  • Aslene (Hong Kong)
  • Orslim
  • Alli® (Orlistat 60mg capsules)
  • Oliet
  • Aliduet (by Mexican pharmaceutical company – Laboratorio Rimsa)
  • Figurin (120 mg)
  • Redicres (by the Venezuelan pharmaceutical company Letifem in capsules at two strengths)
  • Zerotex

Side effects of Orlistat

The terms “adverse reactions” and “side effects” are generally interchangeable.

However, physicians use the term “adverse reactions” implying the patient’s response to a particular drug, while “side effects” are the result of the drug action on the patient’s body.

Since Orlistat affects only the digestive system, main side effects occur mainly in the gastrointestinal tract, i.e. have exclusively local in nature. The negative impact of Orlistat is associated with pharmacokinetic mechanism of the drug preventing the absorption of fats from foods.

Very often, there are such side effects as oily discharge from the rectum, pain and discomfort in the stomach and loose stools.

Herewith, Orlistat is not toxic, since it does not destroy the intestinal mucosa.

In addition to the digestive system, Orlistat extremely rarely, but still may cause side effects affecting other body systems, such as:

  • headaches,
  • respiratory tract infections,
  • hypoglycemia.

Severe form of Orlistat side effects, such as nausea or vomiting is almost not observed in patients with obesity.

When taking the drug, all negative reactions are mainly mild and do not cause much discomfort in the patient.

While using Orlistat, all adverse reactions of the body are mainly transient and their frequency is usually reduced in the second year of treatment in obese patients.

All side effects of Orlistat are manifestation of the action mechanism of the drug on the patient’s body, so they do not cause any harm to health.

Orlistat Contraindications

Children and elderly people did not participate in clinical studies.

Orlistat efficacy and safety in children and the elderly is not known.

Therefore, the drug is contraindicated in children under 12 and people over 65 years.

It should be noted that Orlistat (Xenical) is allowed for use in the pediatric age over 12 years.

Orlistat (Alli) drug is prescribed to adolescents over 16 years of age.

Unlike other weight loss drugs, this medication has just a few contraindications:

  • Hypersensitivity to Orlistat or other drug ingredients;
  • Chronic malabsorption syndrome;
  • Cholestasis;
  • Pregnancy and lactation;
  • Pediatric age to 12 years;
  • Elderly age over 65 years.

Use of this weight loss medication in people with hypersensitivity to the drug ingredients may increase the risk of side effects, such as rash, itching, abdominal pain, fecal incontinence and other gastrointestinal disorders.

Anti-obesity therapy with these diet pills in people with malabsorption syndrome, enhances clinical manifestations (diarrhea, steatorrhea, polyhypovitaminosis, weight loss), which develop as a result of small intestine digestive and transport malfunction.

Inability to absorb food and nutrients contributes to pathological changes in metabolism.

Before you take Orlistat, it is recommended to inform your doctor about any changes that you notice in your health condition at the moment.

For example, itching, change in urine or feces, can be cholestasis symptoms.

This condition is characterized by the reducing of bile amount entering duodenum.

The flow of bile can be reduced due to disorders in bilification or bile flow.

Orlistat and cardiovascular problems

It is important that, unlike appetite suppressants, Orlistat does not affect your heart.

The most common side effects of the fat blocker are abdominal pain, bloating and diarrhea.

The fats that Orlistat blocks in the gastrointestinal tract is excreted in the feces.

Therefore, side effects of Orlistat are explained by changes in activity of digestive enzymes.

No one likes to have any side effects, even if these are insignificant.

Typically, control of fatty food intake helps to minimize risk of side effects.

Orlistat in pregnancy and lactation

The FDA attributed Orlistat drug to category X during pregnancy.

Taking category X drugs before and during pregnancy is contraindicated.

In clinical studies in animals given high Orlistat doses, were not revealed evidence of teratogenicity and embryotoxicity.

Pregnant women did not take part  in Orlistat safety and efficacy clinical studies.

Given that there is no controlled data on Orlistat effect on human pregnancy, it is contraindicated in this period.

Women of reproductive age are recommended to use effective contraception methods while taking Orlistat.

If pregnancy happens during Orlistat use, it is recommended to stop taking this weight loss drug and seek medical advice.

Nursing mothers did not take part in Orlistat research.

Therefore, there is no clinical data on Orlistat excretion in breast milk and its use during lactation is contraindicated.

Orlistat Drug Interactions

Orlistat may alter pharmacological effects or pharmacokinetic parameters of some drugs.

Drug interaction manifests when taking Orlistat with such drugs.

Simultaneous Orlistat use with some drugs can lead to drugs action intensification, as well as to Orlistat toxicity or both drugs.

Orlistat and Cyclosporine

Data from Orlistat and Cyclosporine interaction studies indicate that the simultaneous use of these drugs lowers plasma Cyclosporine levels.

Therefore, Cyclosporine and Orlistat should not be taken simultaneously.

Cyclosporine is recommended to be taken 3 hours after Orlistat intake.

Orlistat and fat-soluble vitamin supplements and their analogues.

Pharmacokinetic interaction studies have shown that the use of Orlistat reduces the absorption of beta-carotene supplements.

Orlistat also slows down the absorption of vitamin E.

Orlistat interaction with the absorption of A, D and K vitamins supplements are not known.

Vitamins A, D, E, K and beta-carotene are advised to be taken 2 hours before or after Orlistat capsules intake.

Orlistat and Levothyroxine

Post-marketing studies have shown that the simultaneous Orlistat and Levothyroxine use increases the risk of hypothyroidism.

Therefore, people taking Orlistat in combination with Levothyroxine drug are recommended to control changes in thyroid function.

If Levothyroxine cannot be canceled for the period of Orlistat use, then these drugs should be taken separately.

Make at least a 4-hour pause between Orlistat and Levothyroxine intake.

Orlistat and Warfarin

During the obesity treatment, people who are prescribed long-term Warfarin use, are recommended to monitor changes in blood clotting.

Orlistat reduces the therapeutic effect of Warfarin (inhibits the synthesis of vitamin K-dependent coagulation factors and anticoagulant proteins C and S in liver).

Orlistat and hypoglycemic drugs

Weight loss during the obesity treatment with Orlistat can have a positive impact on glycemic control in people with diabetes.

Therefore, some patients may need to decrease dosage of their oral hypoglycemic drugs during the anti-obesity therapy.

Orlistat dependence

As with any other weight loss drugs, there is a potential for dependence development while using Orlistat.

The risk of Orlistat drug dependence is highest in people with anorexia nervosa or bulimia.

At that, the very dependence will not be formed by the active substance of the medication, but by the need of a person to  continue .

Orlistat In Different Countries

  • Argentina
  • Australia
  • Austria
  • Belgium
  • Bosnia and Herzegovina
  • Brazil
  • Bulgaria
  • Canada
  • Chile
  • Costa Rica
  • Croatia
  • Czech Republic
  • Denmark
  • El Salvador
  • Estonia
  • Finland
  • France
  • Germany
  • Hong Kong
  • Hungary
  • Iceland
  • India
  • Ireland
  • Israel
  • Italy
  • Latvia
  • Lithuania
  • Luxembourg
  • Madagascar
  • Malaysia
  • Malta
  • Mexico
  • Moldova
  • New Zealand
  • Norway
  • Panama
  • Peru
  • Philippines
  • Poland
  • Portugal
  • Romania
  • Serbia
  • Singapore
  • Slovakia
  • Slovenia
  • South Africa
  • South Korea
  • Spain
  • Sweden
  • Switzerland.

Orlistat Without Prescription

In February 2007, the FDA approved Alli (Orlistat) for sale without prescription.

A distinctive feature of Alli is that it contains two times less amount of active substance than Xenical does.

Low content of active substance almost 100% eliminates risk of moderate or severe side effects.

Just as Xenical, Alli blocks absorption of fat in the body by preventing breakdown of fat molecules.

Both drugs should be taken before, during or immediately after eating.

No more than three pills should be taken per day.

Health experts believe that attractiveness of Alli 60 mg capsules for treatment of severe obesity is lower than that of Xenical 120mg capsules.

Considering, though, that most people suffer from overweight or mild obesity, it is clear why the popularity of OTC doses of Orlistat 60mg has increased sharply.

In order to buy Orlistat 120mg diet pills, a doctor’s prescription is required.

Getting a prescription may take a lot of time.

Furthermore, additional medical examination can be recommended.

Although, this procedure will not be superfluous in case of some diseases of the intestine

Supporters of OTC diet pills Alli believe that this drug is not only safe, but also a cheap alternative to Xenical.

This is true, especially if we take into account that there are no other Orlistat-containing drugs at the US pharmacies.

A different situation has developed in the EU.

The European manufacturers of Orlistat 60mg and 120mg capsules are dozens of pharmaceutical companies that seek to occupy their niche at the market.

High competition on the market of weight loss products led to a sharp decrease in prices on Orlistat-containing drugs.

Manufacturers

Orlistat GSK, Orlistat La Sante, Orlistat Hexal, Orlistat Sandoz, Orlistat Polpharma, Orlistat Teva, Orlistat ratiopharm.